Methylamine → HCID 86656741, compound

Participants

Reaction Steps

[step 1] (E)-{2-[2-(2-Carboxyethyl)-4-methyl-6-phenylbenzimidazol-1-yl]methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene}acetonitrile (100 mg, 0.19 mmol) obtained in Example 62, step 1 was dissolved in DMF (1 mL), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (527 mg, 2.75 mmol), 1-hydroxybenzotriazole (421 mg, 2.75 mmol) and methylamine (2 mol/L THF solution; 0.38 mL, 0.72 mmol) were added, and the mixture was stirred at room temperature for 24 hr. Saturated aqueous sodium hydrogen carbonate solution and water were added to the mixture, and the precipitated solid was collected by filtration to give (E)-{2-[2-(methylcarbamoylethyl)-4-methyl-6-phenylbenzimidazol-1-yl]methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene}acetonitrile (102 mg, 100%).

Provenance & Evidence